HR-LCMS and evaluation of anti-diabetic activity of Hemidesmus indicus (anantmool): Kinetic study, and molecular modelling approach.

This study delved into the exploration of novel antidiabetic medications acquired from natural resources, utilizing the Ayurvedic Rasayana herb Hemidesmus indicus through cutting-edge chemoprofiling and molecular modelling techniques. The methanolic extract of Hemidesmus indicus root exhibited the highest extractive yield (24.70 ± 0.08 %) and contained substantial levels of total phenolic and flavonoid content as 154.15 ± 1.24 mg Gallic Acid Equivalent/g extract and 70.61 ± 0.35 Quercetin Equivalent/g extract respectively. Invitro study revealed the potent inhibitory potential of methanolic extract of the herb against essential carbohydrate hydrolytic enzymes α-amylase (IC50 = 4.19 ± 0.04 mg/ml) and α-glucosidase (IC50 = 5.78 ± 0.10 mg/ml). Further, the enzyme kinetic study demonstrated the competitive mode of inhibition of both enzymes. HR-LCMS analysis identified the major phytoconstituents present in the extracts, including Solanocapsine, Cyclovirobuxine C, Lucidine B, Zygadenine, Aspidospermidine, silychristin, 3beta-3-Hydroxy-18-lupen-21-one, Manglupenone, and 19-Noretiocholanolone. Molecular docking, molecular dynamic simulation, and MM/GBSA analysis have proved stable, rigid, compact, and folded form of complexes during the entire 100 ns simulation, illustrating Zygadenine, Solanocapsine, and Cyclovirobuxine C as the superior inhibitors of α-A protein, while Zygadenine, Plumieride, and Phlegmarine exhibited greater inhibitory behaviour towards α-G protein than the FDA-approved drug acarbose. Collectively, our findings indicate that the Hemidesmus indicus could be a promising source of α-A and α-G inhibitors, potentially serving as a lead in order to develop medications for type-2 diabetes.

An In Silico Molecular Modelling-Based Prediction of Potential Keap1 Inhibitors from Hemidesmus indicus (L.) R.Br. against Oxidative-Stress-Induced Diseases.

The present study investigated the antioxidant potential of aqueous methanolic extracts of Hemidesmus indicus (L.) R.Br., followed by a pharmacoinformatics-based screening of novel Keap1 protein inhibitors. Initially, the antioxidant potential of this plant extract was assessed via antioxidant assays (DPPH, ABTS radical scavenging, and FRAP). Furthermore, 69 phytocompounds in total were derived from this plant using the IMPPAT database, and their three-dimensional structures were obtained from the PubChem database. The chosen 69 phytocompounds were docked against the Kelch-Neh2 complex protein (PDB entry ID: 2flu, resolution 1.50 Å) along with the standard drug (CPUY192018). H. indicus (L.) R.Br. extract (100 µg × mL-1) showed 85 ± 2.917%, 78.783 ± 0.24% of DPPH, ABTS radicals scavenging activity, and 161 ± 4 µg × mol (Fe (II)) g-1 ferric ion reducing power. The three top-scored hits, namely Hemidescine (-11.30 Kcal × mol-1), Beta-Amyrin (-10.00 Kcal × mol-1), and Quercetin (-9.80 Kcal × mol-1), were selected based on their binding affinities. MD simulation studies showed that all the protein-ligand complexes (Keap1-HEM, Keap1-BET, and Keap1-QUE) were highly stable during the entire simulation period, compared with the standard CPUY192018-Keap1 complex. Based on these findings, the three top-scored phytocompounds may be used as significant and safe Keap1 inhibitors, and could potentially be used for the treatment of oxidative-stress-induced health complications.

Elicitor mediated enhancement of shoot biomass and lupeol production in Hemidesmus indicus (L.) R. Br. ex. Schult. and Tylophora indica (Burm. F.) Merrill using yeast extract and salicylic acid.

Hemidesmus indicus (L.) R. Br. ex Schult. and Tylophora indica (Burm. F.) Merrill shoot cultures were treated with different concentrations of yeast extract (YE; 25-200 mg/L) and salicylic acid (SA; 50-200 µM), and their effect on lupeol production was assessed. The maximum dry weight (DW) biomass was recorded when H. indicus shoots were treated with SA (50 µM) and T. indica shoots with YE (200 mg/L). Highest lupeol yield (335.40 ± 0.04 µg/g DW) was obtained in H. indicus shoots after treatment with 50 µM of SA for 3 weeks. Whereas in T. indica, maximum lupeol content (584.26 ± 8.14 µg/g DW) was recorded by giving treatment with 25 µM of SA for 6 weeks.

Methanolic extract of Hemidesmus indicus root augments the antibacterial and antibiofilm activity of amoxicillin and clindamycin against methicillin-resistant Staphylococcus aureus of bovine origin.

The present study evaluated the antibacterial and antibiofilm activity of methanolic extract of Hemidesmus indicus root (MHIR) in combination with amoxicillin and clindamycin against biofilm-forming methicillin-resistant Staphylococcus aureus (MRSA) isolated from milk samples of mastitic cows. Microdilution susceptibility testing and microtitre plate assays were used to evaluate the in vitro efficacy of MHIR and antibiotic combinations against MRSA (n = 12). Furthermore, in vitro findings were validated in a murine model. Minimum inhibitory concentration and minimum biofilm inhibitory concentration of amoxicillin and clindamycin in combination with MHIR were significantly (P < 0·05) lower than when used alone against MRSA. In terms of antibacterial activity, MHIR showed additive interaction (fractional inhibitory concentrationindex >0·5-4) with amoxicillin and clindamycin against all the MRSA isolates, whereas MHIR synergizes (fractional biofilm inhibitory concentrationindex ≤0·5) the antibiofilm activity of amoxicillin and clindamycin against 58·33% and 83·33% of the MRSA isolates respectively. Amoxicillin/clindamycin in combination with MHIR significantly (P < 0·05) reduced disease activity score, and bacterial load and Gram-positive spots in kidney and liver of MRSA-infected mice. The combined efficacy of MHIR and amoxicillin/clindamycin was comparable to clindamycin alone but superior to amoxicillin alone. Hence, the combination of MHIR with amoxicillin/clindamycin is advocated in the treatment of MRSA-associated infections.

Box-Behnken design avenue for development and validation of high-performance thin-layer chromatography method for estimation of rutin in Hemidesmus indicus.

The aim of this study was to determine the content of rutin in Hemidesmus indicus and to optimize the high-performance thin-layer chromatography method. The method was validated in compliance with the International Council for Harmonisation guidelines Q2 (R1) for parameters such as linearity, accuracy, precision, robustness, limit of detection, and limit of quantitation. A Box-Behnken design and response surface methodology has been used to investigate the impact of independent variables on the response. Three independent variables, mobile phase composition (% v/v), mobile phase volume (mL), and duration of saturation (min), were studied. Rutin was verified, and its content was determined using a validated high-performance thin-layer chromatography method with good linearity within the range of 200-1000 ng spot-1 with r2 = 0.9998 and correlation coefficient with calibration curve equation y = 0.0297x + 0.0001. The average percentage recovery values varied from 99.03 to 101.15 and 98.88 to 100.12%, respectively, for in-house and marketed mother tincture). The peak area determination at three different concentration levels shows low values of percentage relative standard deviation (<2%) for inter-day (0.04-0.06) and intra-day (0.04-0.05) precision of rutin. The average content of rutin in extract and marketed mother tincture was 229 ± 0.57 and 210 ± 0.57 µg g-1 . The proposed method was simple, precise, and accurate for the determination of rutin with frequent quality control assessment of H. indicus.

Hemidesmus indicus L. Br.: critical assessment of in vitro biotechnological advancements and perspectives.

Hemidesmus indicus (L.) R. Br. ex Schult., commonly known as Indian sarsaparilla or Anantamul, is an ethnopharmacologically important medicinal plant from the family Apocynaceae. Biosynthesis of an array of bioactive compounds such as methoxybenzaldehydes and their derivatives has been accountable for its intensive medicinal attributes. Low seed setting, over-exploitation from natural habitat and a need for selection and preservation of elite germplasms yielding higher levels of bioactive compounds have led researchers to enquire the standardization of micropropagation techniques and quantitative estimation of phytochemicals from H. indicus. The present work aims to have a comprehensive account on micropropagation in H. indicus, a comparative estimation of biotic and abiotic factors, viz. elicitors and precursors playing a crucial role in H. indicus tissue culture, a critical appraisal of applied protocols to nullify embellished claims and a discussion on future perspectives. The review also highlights the comparative effect of different plant growth regulators as well as their combined role in rhizogenesis, callogenesis, base callus formation, callusing and somatic embryo-mediated indirect organogenesis, outcome of explant selection, contribution of abiotic (temperature, photoperiod, moisture, inorganic molecules) factors, role of carbon source, application of sterilization techniques and associated success rates, role of factors essential for acclimatization and secondary metabolite production, synthetic seed production and genetic transformation techniques. The compiled information along with individual study details, respective outcome and variability of reports will aid in proper assessment of cited standardized tissue culture protocols in H. indicus especially in relation to secondary metabolite production. Moreover, the assessment of applicability of different methodologies in this aspect will aid in the selection of high-yielding germplasms or chemotypes which is not only profitable for industrial application but also important for basic and applied preclinical and clinical research studies. KEY POINTS: • Critical and updated assessment on in vitro biotechnology in Hemidesmus indicus. • Biotechnological advancement via Agrobacterium-mediated transformation. • Key shortcomings and future research directions Graphical abstract Effect of biotic and abiotic factors on Micropropagation and secondary metabolite synthesis in Hemidesmus indicus.

Indian sarsaparilla, Hemidesmus indicus (L.) R. Br. ex Schult: tissue culture studies.

Hemidesmus indicus (L.) R. Br. ex Schult is commonly known as anantmul or Indian sarsaparilla. The roots of this plant, which display a wide range of medicinal, biological, and phytopharmaceutical properties, are used in the pharmaceutical and food industries. Conventionally, the plant is propagated by seed germination or vegetatively, but the efficacy of traditional methods has some limitations: plants derived from seed germination are prone to seed-borne diseases, or plantlet production using vegetative propagation is limited. In contrast, plant tissue culture allows for large-scale propagation and secondary metabolite production in vitro without sacrificing plants from their natural habitats. Many efforts have been made over 40 years of research to establish efficient micropropagation protocols to speed up cultivation of this plant, including callus-mediated in vitro propagation, somatic embryogenesis, and shoot multiplication using cotyledenory nodes, stem segments, shoot tips, and nodal explants. Among these explants, nodal explants are the most commonly used for H. indicus micropropagation. The application of adenine sulfate, citric acid, ascorbic acid, and arginine may be useful in preventing explant browning, premature leaf senescence, and shoot tip abscission during in vitro culture. This review provides insight into micropropagation, use of synthetic seeds for short-term germplasm preservation, and in vitro production of secondary metabolites such as 2-hydroxy-4-methoxybenzaldehyde, lupeol, vanillin, and rutin, from in vitro root and callus cultures. Furthermore, unexplored and possible innovative areas of research in Hemidesmus biotechnology are also discussed. KEY POINTS: • Hemidesmus indicus has multiple therapeutic applications. • H. indicus roots are used in confectionary and pharmacy. • This review comprehensively assesses H. indicus tissue culture. • Challenges and future research of H. indicus biotechnology are discussed.

2-Hydroxy-4-methoxybenzaldehyde from Hemidesmus indicus is antagonistic to Staphylococcus epidermidis biofilm formation.

Staphylococcus epidermidis (SE) is an opportunistic nosocomial pathogen that accounts for recalcitrant device-related infections worldwide. Owing to the growing interest in plants and their secondary metabolites targeting bacterial adhesion, this study was intended to uncover the anti-biofilm potential of Hemidesmus indicus and its major constituent 2-hydroxy-4-methoxybenzaldehyde (HMB) against SE. The minimum biofilm inhibitory concentration (MBIC) of H. indicus root extract and HMB were found to be 500 and 250 µg ml-1, respectively. The results of time-dependent biofilm inhibition and mature biofilm disruption assays confirmed that HMB targets initial cell adhesion. Furthermore, interference by HMB in the expression of adhesin genes (icaA, aap and bhp) and biofilm components was associated with an increased susceptibility of SE to oxidative stress and antibiotics. To conclude, this study reports for the first time HMB as a potential drug against SE biofilms.

Indian Sarsaparilla (Hemidesmus indicus): Recent progress in research on ethnobotany, phytochemistry and pharmacology.

ETHNOPHARMACOLOGICAL RELEVANCE: Hemidesmus indicus (L.) R. Br. ex Schult. (Apocynaceae) is widely used in traditional medicine in the different parts of the Indian subcontinent due to the various biological activities attributed to its different parts, especially the roots. It has traditionally been used for treating snakebites, scorpion stings, diabetes, urinary diseases, dyspnea, menorrhagia, oligospermia, anorexia, fever, abdominal colic and pain, dysentery, diarrhea, cough, rheumatism, headache, inflammation, pyrosis, skin diseases, leprosy, sexually transmitted diseases and cancer. In Ayurveda, the plant is used in the treatment of bone-loss, low body weight, fever, stress, topical wound and psoriasis. Besides, Ayurvedic literature also depicts its use as anti-atherogenic, anti-spasmodic, memory enhancing, immunopotentiating and anti-inflammatory agents. AIM OF THE STUDY: In this review, we aim to present a comprehensive update on the ethnopharmacology, phytochemistry, specific pharmacology, and toxicology of H. indicus and its bioactive metabolites. Possible directions for future research are also outlined in brief. MATERIALS AND METHODS: Popular and widely used international databases such as PubMed, Scopus, Science Direct, Google Scholar and JSTOR were searched and traditional literature were consulted using the various search strings to retrieve a number of citations related to the ethnopharmacology, biological activity, toxicology, quality control and phytochemistry of H. indicus. All studies on the ethnobotany, phtochemistry, pharmacology, and toxicology of the plant up to 2019 were included in this review. RESULTS: H. indicus has played an important role in traditional Indian medicine (including Ayurveda) and also in European medicine. The main pharmacological properties of H. indicus include hepatoprotective, anti-cancer, anti-diabetic, antioxidant, neuroprotective, anti-ophidian, cardioprotective, nephroprotective, anti-ulcerogenic, anti-inflammatory, and antimicrobial properties. Phytochemical evaluations of the root have revealed the presence of aromatic aldehydes and their derivatives, phenolics, triterpenoids and many other compounds, some of which were attributed to its bioactivity. This review also compiles a list of Ayurvedic formulations and commercial preparations where H. indicus has been used as an active ingredient. We have included the critical assessment of all the papers cited in this manuscript based on experimental observation and other important points which reflect the loop-holes of research strategy and ambiguity in the papers reviewed in this manuscript. CONCLUSIONS: The study presents an exhaustive and updated review on the traditional, pharmacological and phytochemical aspects of H. indicus with notes on its quality control and toxicological information. Although the crude extracts of H. indicus exhibit an array of pharmacological activities, it is high time to identify more active phyto-constituents by bioactivity-guided isolation besides elucidating their structure-activity relationship. More designed investigations are needed to comprehend the multi-target network pharmacology, to clarify the molecular mode of action and to ascertain the efficacious doses of H. indicus. Moreover, H. indicus is not fully assessed on the basis of its safety and efficacy on human. We hope this review will compile and improve the existing knowledge on the potential utilization of H. indicus in complementary and alternative medicine.

In Silico Studies on Anti-Stress Compounds of Ethanolic Root Extract of Hemidesmus indicus L.

BACKGROUND: Alternative medicine is available for those diseases which cannot be treated by conventional medicine. Ayurveda and herbal medicines are important alternative methods in which the treatment is done with extracts of different medicinal plants. This work is concerned with the evaluation of anti-stress bioactive compounds from the ethanolic root extract of Hemidesmus indicus. METHODS: Gas chromatography and Mass Spectrum studies are used to identify the compounds present in the ethanolic extract based on the retention time, area. In order to perform docking studies, Vasopressin model is generated using modeling by Modeller 9v7. Vasopressin structure is developed based on the crystal structure of neurophysin-oxytocin from Bos taurus (PDB ID: 1NPO_A) collected from the PDB data bank. Using molecular dynamics simulation methods, the final predicted structure is obtained and further analyzed by verifying 3D and PROCHECK programs, confirmed that the final model is reliable. The identified compounds are docked to vasopressin for the prediction of anti-stress activity using GOLD 3.0.1 software. RESULTS: The predicted model of Vasopressin structure is stabilized and confirmed that it is a reliable structure for docking studies. The results indicated ARG4, THR7, ASP9, ASP26, ALA32, ALA 80 in Vasopressin are important determinant residues in binding as they have strong hydrogen bonding with phytocompounds. Among the 21 phytocompounds identified and docked, molecule Deoxiinositol, pentakis- O-(trimethylsilyl) showed the best docking results with Vasopressin. CONCLUSION: The identified compounds were used for anti-stress activity by insilico method with Vasopressin which plays an important role in causing stress and hence selected for inhibitory studies with phytocompounds. The phytocompounds are inhibiting vasopressin through hydrogen bodings and are important in protein-ligand interactions. Docking results showed that out of twenty-one compounds, Deoxiinositol, pentakis-O-(trimethylsilyl) showed best docking energy to the Vasopressin.

Hemidesmus indicus induces apoptosis via proteasome inhibition and generation of reactive oxygen species.

Proteasome inhibition represents an important anticancer strategy. Here, we studied the mechanisms at the basis of the pro-apoptotic activity of the standardized decoction of Hemidesmus indicus, a plant evoking a complex anticancer activity, and explored its inhibition of proteasome activity in human leukemia cells. Additionally, we preliminary tested the cytotoxicity of some H. indicus's phytochemicals on leukemia cells and their intestinal absorption on a human intestinal epithelium model consisting of a monolayer of differentiated Caco2 cells. We observed a potent antileukemic effect for H. indicus, imputable to the modulation of different critical targets at protein and mRNA levels and the reduction of the 26S proteasome expression. We found that some phytomarkers of H. indicus decoction passed through the enterocyte monolayer. Overall, our study supports the pharmacological potential of H. indicus, which can represent an interesting botanical drug in the oncological area.

Seasonal deviation effects foliar endophyte assemblage and diversity in Asparagus racemosus and Hemidesmus indicus.

BACKGROUND: Fungal endophytes are the living symbionts which cause no apparent damage to the host tissue. The distribution pattern of these endophytes within a host plant is mediated by environmental factors. This study was carried out to explore the fungal endophyte community and their distribution pattern in Asparagus racemosus and Hemidesmus indicus growing in the study area. RESULTS: Foliar endophytes were isolated for 2 years from A. racemosus and H. indicus at four different seasons (June-August, September-November, December-February, March-May). A total of 5400 (675/season/year) leaf segments harbored 38 fungal species belonging to 17 genera, 12 miscellaneous mycelia sterile from 968 isolates and 13 had yeast like growth. In A. racemosus, Acremonium strictum and Phomopsis sp.1, were dominant with overall relative colonization densities (RCD) of 7.11% and 5.44% respectively, followed by Colletotrichum sp.3 and Colletotrichum sp.1 of 4.89% and 4.83% respectively. In H. indicus the dominant species was A. strictum having higher overall RCD of 5.06%, followed by Fusarium moniliforme and Colletotrichum sp.2 with RCD of 3.83% and 3%, respectively. Further the overall colonization and isolation rates were higher during the wet periods (September-November) in both A. racemosus (92.22% and 95.11%) and H. indicus (82% and 77.11%). CONCLUSION: Study samples treated with 0.2% HgCl2 and 75% EtOH for 30 s and 1 min, respectively, confirmed most favorable method of isolation of the endophytes. Owing to high mean isolation and colonization rates, September-November season proved to be the optimal season for endophyte isolation in both the study plants. Assessing the bioactive potential of these endophytes, may lead to the isolation of novel natural products and metabolites.

Hemidesmus indicus (L.) R. Br. extract inhibits the early step of herpes simplex type 1 and type 2 replication.

Herpes simplex virus types 1 (HSV-1) and 2 (HSV-2) cause several clinically relevant syndromes in both adults and neonates. Despite the availability of efficient anti-HSV agents, the search for new therapeutic approaches is highly encouraged due to the increasing drug resistance of virus strains. Medicinal plants represent a source of potential bioactive compounds. In this context we evaluated the anti-herpetic activity of Hemidesmus indicus (L.) R. Br., a plant widely used in traditional Indian medicine. The hydroalcoholic extract prepared from roots was characterized by NMR and HPLC analysis and assayed in vitro by CPE reduction and virus infectivity assays to define its anti-viral effect. The extract's mechanism of action was investigated by virucidal and time-of-addition assays and by in vitro α-glucosidase inhibitory assay. The extract exhibited a remarkable anti-herpetic activity at 100 mg/mL, at non-cytotoxic concentration, through multiple mechanisms: it reduced the infectivity of viral particles released from infected cells possibly through its anti-ER α-glucosidase inhibitory activity and it inhibited the beginning stage of HSV infection acting as a virucide agent and/or preventing virus attachment to the host cell surface.

In Vitro Study of the Cytotoxic, Cytostatic, and Antigenotoxic Profile of Hemidesmus indicus (L.) R.Br. (Apocynaceae) Crude Drug Extract on T Lymphoblastic Cells.

In traditional Indian medicine, the crude drug Hemidesmus indicus root-commonly known as Indian sarsaparilla-is used alone or in poly-herbal preparations for the treatment of a wide range of diseases. The present study focuses on the cancer chemopreventive and therapeutic potential of H. indicus extracts on an acute lymphoblastic leukemia cell line (CCRF-CEM). With this aim in mind, we subjected H. indicus roots to two subsequent extractions (hydro-alcoholic extraction and soxhlet extraction). As DNA damage is an important prerequisite for the induction of mutations/cancer by genotoxic carcinogens, cancer chemoprevention may be achieved by preventing genotoxicity. Through an integrated experimental approach, we explored the genoprotective potential of the soxhlet H. indicus extract against different mutagenic compounds and its cytotoxic, proapoptotic, and cytostatic properties. In our experimental conditions, H. indicus induced a cytotoxic effect involving the activation of both intrinsic and extrinsic apoptotic pathways and blocked the cell cycle in the S phase. Moreover, the antigenotoxicity results showed that the extract was able to mitigate DNA damage, an essential mechanism for its applicability as a chemopreventive agent, via either the modulation of extracellular and intracellular events involved in DNA damage. These data add to the growing body of evidence that H. indicus can represent a noteworthy strategy to target early and late stages of cancer.

Delaying of cataract through intervention of Hemidesmus indicus in STZ induced diabetic rats.

Hemidesmus indicus (L.) R. Br. was extensively used as hypoglycaemic agent and significance of this plant on secondary complications of diabetes remained unknown. The present study was to investigate the anti-cataractous activity of H. indicus against streptozotocin (STZ)-induced diabetic cataract in rodent model. Root extracts have been prepared and tested for inhibition of rat lens aldose reductase (AR) activity. In addition, its pharmacological potential has been investigated in STZ-induced diabetic cataract. Methanol extract of H. indicus-inhibited AR activity in vitro decreased the blood glucose levels, inhibited the AR activity and delayed the onset and progression of cataract in a dose-dependent manner in in vivo and the antioxidant markers have been normalised. Our results demonstrate that H. indicus has decrease the osmotic stress by inhibiting the AR activity and prevented the loss of antioxidants and delayed the progression of diabetic cataract in STZ-induced diabetic rats.

Antiaflatoxigenic and Antimicrobial Activities of Schiff Bases of 2-Hydroxy-4-methoxybenzaldehyde, Cinnamaldehyde, and Similar Aldehydes.

2-Hydroxy-4-methoxybenzaldehyde (HMBA) is a nontoxic phenolic flavor from dietary source Decalipus hamiltonii and Hemidesmus indicus. HMBA is an excellent antimicrobial agent with additional antiaflatoxigenic potency. On the other hand, cinnamaldehyde from cinnamon is a widely employed flavor with significant antiaflatoxigenic activity. We have attempted the enhancement of antiaflatoxigenic and antimicrobial properties of HMBA, cinnamaldehyde, and similar molecules via Schiff base formation accomplished from condensation reaction with amino sugar (d-glucamine). HMBA derived Schiff bases exhibited commendable antiaflatoxigenic activity at the concentration 0.1 mg/mL resulting in 9.6 ± 1.9% growth of Aspergillus flavus and subsequent 91.4 ± 3.9% reduction of aflatoxin B1 with respect to control.

Protective Effect of a Polyherbal Aqueous Extract Comprised of Nigella sativa (Seeds), Hemidesmus indicus (Roots), and Smilax glabra (Rhizome) on Bleomycin Induced Cytogenetic Damage in Human Lymphocytes.

This study was carried out to determine the chemoprotective potential of a polyherbal aqueous decoction comprised of Nigella sativa (seeds), Hemidesmus indicus (roots), and Smilax glabra (rhizome) against bleomycin induced cytogenetic damage in human lymphocytes. Isolated peripheral blood lymphocytes (PBLs) were exposed to bleomycin at a dose of 40 µg/mL for 2 hrs in the presence or absence of different doses of the decoction (100, 300, and 600 µg/mL). Modulatory effect of the decoction on bleomycin induced cytogenetic damage was evaluated by (a) degree of chromosomal aberrations (CA), (b) formation of micronuclei (MN), and (c) induction of γH2AX foci in lymphocytes exposed to bleomycin. Lymphocytes pretreated with the decoction showed that a significant reduction (p < 0.05) in bleomycin induced (a) stable and unstable chromosome aberrations (CA), (b) MN formation, and (c) formation of γH2AX foci, when compared to lymphocytes treated only with bleomycin. The decoction by itself did not induce any significant cytogenetic damage in PBLs. Overall results of the present study confirm that the decoction can attenuate the cytogenetic damage mediated by bleomycin in human PBLs.

Multi-target activity of Hemidesmus indicus decoction against innovative HIV-1 drug targets and characterization of Lupeol mode of action.

Despite the availability of several anti-retrovirals, there is still an urgent need for developing novel therapeutic strategies and finding new drugs against underexplored HIV-1 targets. Among them, there are the HIV-1 reverse transcriptase (RT)-associated ribonuclease H (RNase H) function and the cellular α-glucosidase, involved in the control mechanisms of N-linked glycoproteins formation in the endoplasmic reticulum. It is known that many natural compounds, such as pentacyclic triterpenes, are a promising class of HIV-1 inhibitors. Hence, here we tested the pentacyclic triterpene Lupeol, showing that it inhibits the HIV-1 RT-associated RNase H function. We then performed combination studies of Lupeol and the active site RNase H inhibitor RDS1759, and blind docking calculations, demonstrating that Lupeol binds to an HIV-1 RT allosteric pocket. On the bases of these results and searching for potential multitarget active drug supplement, we also investigated the anti-HIV-1 activity of Hemidesmus indicus, an Ayurveda medicinal plant containing Lupeol. Results supported the potential of this plant as a valuable multitarget active drug source. In fact, by virtue of its numerous active metabolites, H. indicus was able to inhibit not only the RT-associated RNase H function, but also the HIV-1 RT-associated RNA-dependent DNA polymerase activity and the cellular α-glucosidase.

Antiosteoporotic effect of Hemidesmus indicus Linn. on ovariectomised rats.

PHARMACOLOGICAL RELEVANCE: Root of Hemidesmus indicus (L). R. Br., an herbal drug of India is traditionally used to prevent or treat female hormonal disturbance related disorders and assuaging symptoms of menopausal conditions. AIM OF THE STUDY: Lack of scientific data for potential use in bone loss, the present study was undertaken to investigate the effects of ethanol extract of Hemidesmus indicus root for osteoporosis in ovariectomised rats. MATERIALS AND METHODS: Thirty wistar female rats were randomly divided into five groups. One group was sham operated and other four groups were undergone dorsal ovariectomy (OVX). After four weeks of post-operative recovery, three OVX groups, viz. Group1, Group2 and Group3 were treated for ninety days with standard raloxifene (RLX) 1mg/kg/day, Hemidesmus indicus root extract (HIRE) 100mg/kg/day and HIRE 200mg/kg/day respectively. Sham and OVX control groups were fed with equal 1% vehicle volume. Serum and urine biochemistry (alkaline phosphatase, tartrate resistant acid phosphatase, triglyceride, total cholesterol, calcium, phosphorous and hydroxyproline), weight of body, uterus and vagina, femur parameters, three point bending of tibia and fourth lumbar vertebra compression were examined. Furthermore, bone architecture and uterine hypertrophy were examined by histopathological studies. RESULTS: Application of HIRE has increased bone strength and restored bone turnover markers such as alkaline phosphatase, tartrate resistant acid phosphatase and hydroxyproline moreover, improved femur parameters indicated mineralized bones, similar to the results observed with raloxifene treatment. Histopathology studies showed fibrocartilaginous proliferation of trabecular bone and absence of uterine hypertrophy. CONCLUSION: The results strongly suggest that HIRE prevents bone loss in OVX induced osteoporosis without estrogen like side effects. It might be a potential remedy like raloxifene for postmenopausal or estrogen deficiency caused osteoporosis.

Anti-Psychotic Activity of Aqueous Root Extract of Hemidesmus indicus: A Time Bound Study in Rats.

AIMS AND BACKGROUND: Psychosis is a neurological disorder, which is usually defined as the &quot;loss of contact with reality.&quot; As medicine 'Hemidesmusindicus' holds a reputed place in all systems of medicine in India. It is given in the form of infusion, fine particles, or syrup. It is also a component of several medicinal preparations. The present research work is pertaining to find out an anti-psychotic activity of an aqueous root extract of Hemidesmusindicus- a time bound study in rats. METHODS: In the present study, the dried roots of Hemidesmusindicus were crushed to a coarse powder and extracted with water under reflux for 36 hours to obtain the aqueous extract of roots of Hemidesmusindicus (AERHI). The extract was reconstituted in 2% aqueous tragacanth just before use and administered orally at a dose 0f 100 mg/kg, 300 mg/kg and 500 mg/kg. In a single dose study, the parameters were assessed after oral administration of the single dose of the AERHI, whereas in a multiple dose study, the animals daily received the suitable oral dose of the AERHI for a period of 30 days. The parameters were assessed on the 15th and 30th day. The antipsychotic activity was screened using Apomorphine induced Stereotyped behavior in rats and Haloperidol induced catalepsy models were used. In Apomorphine induced Stereotyped behavior inhibition of the Stereotyped behavior was considered to be anti-psychotic activity and in Haloperidol induced catalepsy, we observed whether the AERHI potentate or attenuate the catalepsy in rats. RESULTS: In this study, the extract of Hemidesmusindicus significantly inhibited the stereotyped behavior induced by apomorphine in rats and also potentiate the catalepsy induced by haloperidol, thereby showing its anti-psychotic activity. CONCLUSION: All these observations imply that Hemidesmusindicus extract possesses anti-psychotic activity in experimental animals.